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1.
Xenobiotica ; 6(3): 159-69, 1976 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-1274380

RESUMO

1. After administration of dl-alpha-methylfluorene-2-acetic acid to dogs, the optical rotation of the drug in blood increased with time. Of the total drug in blood, the d-enantiomer increased from 61 to 80% between 3 and 24 h after administration; by 384 h it was 100%. 2. Both l- and d-enantiomers had plasma half-lives and excretion characteristics similar to those of the dl-racemic mixture, indicating that the increase in the proportion of the d-enantiomer was not due to more rapid excretion of the l-enantiomer. 3. Studies of optical rotation and circular dichroism demonstrated that the l-enantiomer was converted to the d-enantiomer in the blood of the dog, but the d-enantiomer remained unchanged. After administration of the l-enantiomer, the d-enantiomer increased from 26 to 71% of the total drug in blood between 0-3 and 2 days after administration; 14 days after dosing, almost all of the drug was present as the d-enantiomer. 4. Isomerization of l-alpha-methylfluorene-2-acetic acid to its d-enantiomer also occurs in rat, monkey and man.


Assuntos
Fluorenos/metabolismo , Isomerases/metabolismo , Acetatos/metabolismo , Animais , Cromatografia em Camada Fina , Dicroísmo Circular , Cães , Feminino , Meia-Vida , Masculino , Conformação Molecular , Rotação Ocular , Estereoisomerismo , Relação Estrutura-Atividade
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